Development of pH sensitive polymeric nanoparticle of erythromycin

Abstract

Introduction: Erythromycin is a macrolide antibiotic used for the treatment of various infections caused by
bacteria. It is also used for Respiratory tract infection, skin infection, syphilis, etc. Erythromycin base was a
poorly water-soluble and acid-labile drug. The bioavailability of Erythromycin was very less about (15–35%). The
absorption site of Erythromycin is the small intestine. pH-responsive polymeric drug delivery system is efficient
delivering the acid instable drugs. Aim: The main objective of the study is to formulate Erythromycin loaded
pH-responsive polymeric nanoparticles was prepared using pHresponsive polymer to prevent the degradation
of acid-labile drug and to evaluate the Polymeric nanoparticle. Materials and Methods: The Erythromycin
Polymeric nanoparticles were prepared by Nano precipitation method using Eudragit L100 as a Polymer and
polyvinyl alcohol (PVA) as stabilizer. The particle size, polydispersity index (PDI), zeta potential, entrapment
efficiency and In-vitro drug release studies were performed for nanoparticle. The compatibility between drug and
polymer was studied by Fourier transform infrared. The nanoparticle was lyophilized and surface morphology
was determined by scanning electron microscope. Excipients were added and formulated into tablet. The
Precompression evaluation of lyophilized powder was carried out. The post-compression evaluation for tablets
and In-vitro release study was performed and compared with marketed tablet. Results: Erythromycin nanoparticle
was formulated and evaluated. It showed the particle size of 270.2 nm with PDI of 0.166 and the zeta potential was
found to be −32.5. The Entrapment efficiency of the ENP 9 Nanoparticle was 96%. Erythromycin loaded tablet
was formulated and evaluated for hardness, weight variation, disintegration, friability, thickness, and diameter. It
was present within the limit. In vitro drug release of the formulated tablet showed 91% drug release in phosphate
buffer pH6.8 at the end of 60 min. Conclusion: Erythromycin nanoparticles were in the nanometer range and it
was stable. Polymeric nanoparticle tablet had the ability to protect the acid-labile drug and it gets dissolved in
the intestine pH 6.8. The nano particulate tablet showed the better release when compared with marketed tablet.